EA201290036A1 - Липидированные производные оксоаденина - Google Patents

Липидированные производные оксоаденина

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Publication number
EA201290036A1
EA201290036A1 EA201290036A EA201290036A EA201290036A1 EA 201290036 A1 EA201290036 A1 EA 201290036A1 EA 201290036 A EA201290036 A EA 201290036A EA 201290036 A EA201290036 A EA 201290036A EA 201290036 A1 EA201290036 A1 EA 201290036A1
Authority
EA
Eurasian Patent Office
Prior art keywords
lipidated
oxoadenine
derivatives
oxoadenine derivatives
oxoadenines
Prior art date
Application number
EA201290036A
Other languages
English (en)
Other versions
EA023536B1 (ru
Inventor
Дэвид Джонсон
Original Assignee
Глаксосмитклайн Байолоджикалс Са
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Глаксосмитклайн Байолоджикалс Са filed Critical Глаксосмитклайн Байолоджикалс Са
Publication of EA201290036A1 publication Critical patent/EA201290036A1/ru
Publication of EA023536B1 publication Critical patent/EA023536B1/ru

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/543—Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
    • A61K47/544—Phospholipids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/554—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
    • A61K47/6905—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion
    • A61K47/6911—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion the form being a liposome
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Botany (AREA)
  • Dispersion Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Новые липидированные оксоаденины, содержащие замещенную азотсодержащим гетероциклилом молекулу оксоаденина, ковалентно связанную с фосфо- или фосфонолипидом, являются, как показано, индукторами интерферона-α и других иммуностимулирующих цитокинов. Соединения полезны в качестве иммуностимуляторов и адъювантов.
EA201290036A 2009-08-07 2010-08-06 Производные оксоаденина, конъюгированные с фосфо- или фосфонолипидами EA023536B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US23213209P 2009-08-07 2009-08-07
PCT/US2010/044703 WO2011017611A1 (en) 2009-08-07 2010-08-06 Lipidated oxoadenine derivatives

Publications (2)

Publication Number Publication Date
EA201290036A1 true EA201290036A1 (ru) 2012-12-28
EA023536B1 EA023536B1 (ru) 2016-06-30

Family

ID=43544685

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201290036A EA023536B1 (ru) 2009-08-07 2010-08-06 Производные оксоаденина, конъюгированные с фосфо- или фосфонолипидами

Country Status (15)

Country Link
US (1) US9044481B2 (ru)
EP (2) EP2461690A4 (ru)
JP (1) JP5759992B2 (ru)
KR (1) KR20120055623A (ru)
CN (1) CN102469790B (ru)
AU (1) AU2010279299B2 (ru)
BR (1) BR112012002349A2 (ru)
CA (1) CA2768195A1 (ru)
EA (1) EA023536B1 (ru)
ES (1) ES2732999T3 (ru)
MX (1) MX2012001524A (ru)
SG (1) SG178237A1 (ru)
TR (1) TR201909600T4 (ru)
WO (1) WO2011017611A1 (ru)
ZA (1) ZA201200646B (ru)

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UA103195C2 (ru) 2008-08-11 2013-09-25 Глаксосмитклайн Ллк Производные пурина для применения в лечении аллергий, воспалительных и инфекционных заболеваний
WO2010088924A1 (en) 2009-02-06 2010-08-12 Telormedix Sa Pharmaceutical compositions comprising imidazoquinolin(amines) and derivatives thereof suitable for local administration
NO2491035T3 (ru) 2009-10-22 2018-01-27
JP2013519644A (ja) 2010-02-10 2013-05-30 グラクソスミスクライン エルエルシー プリン誘導体およびそれらの薬学的使用
AU2011247358B2 (en) 2010-04-30 2014-10-30 Urogen Pharma Ltd. Phospholipid drug analogs
US9050319B2 (en) 2010-04-30 2015-06-09 Telormedix, Sa Phospholipid drug analogs
AU2011247359A1 (en) * 2010-04-30 2012-11-15 Telormedix Sa Methods for inducing an immune response
US10112946B2 (en) 2011-07-22 2018-10-30 Glaxosmithkline Llc Composition
EP2674170B1 (en) 2012-06-15 2014-11-19 Invivogen Novel compositions of TLR7 and/or TLR8 agonists conjugated to lipids
US9555036B2 (en) 2012-08-24 2017-01-31 Glaxosmithkline Llc Pyrazolopyrimidine compounds
PT2922549T (pt) * 2012-11-20 2017-09-01 Glaxosmithkline Llc Novos compostos
WO2014081644A1 (en) 2012-11-20 2014-05-30 Glaxosmithkline Llc Novel compounds
ES2625023T3 (es) 2012-11-20 2017-07-18 Glaxosmithkline Llc Compuestos novedosos
US9295732B2 (en) 2013-02-22 2016-03-29 Invivogen Conjugated TLR7 and/or TLR8 and TLR2 polycationic agonists
WO2015036044A1 (en) * 2013-09-13 2015-03-19 Telormedix Sa Cationic lipid vehicles for delivery of tlr7 agonists for specific targeting of human cd14+ monocytes in whole blood
AR100137A1 (es) 2014-04-22 2016-09-14 Hoffmann La Roche Compuestos 4-amino-imidazoquinolina
CA2967248A1 (en) 2014-11-13 2016-05-19 Glaxosmithkline Biologicals Sa Adenine derivatives which are useful in the treatment of allergic diseases or other inflammatory conditions
LT3265458T (lt) 2015-03-06 2019-03-12 F. Hoffmann-La Roche Ag Benzazepino dikarboksamido junginiai
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EP3350168B1 (en) 2015-09-17 2019-12-18 H. Hoffnabb-La Roche Ag Sulfinylphenyl or sulfonimidoylphenyl benzazepines
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US10632192B2 (en) 2015-10-07 2020-04-28 Sumitomo Dainippon Pharma Co., Ltd. Pyrimidine compounds and their use as vaccine adjuvants
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JP6918838B2 (ja) 2016-05-23 2021-08-11 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 第三級アミド基を有するベンズアゼピンジカルボキサミド化合物
JP7022702B2 (ja) 2016-05-23 2022-02-18 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト 第二級アミド基を有するベンズアゼピンジカルボキサミド化合物
JP7012668B2 (ja) 2016-06-12 2022-02-14 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト ジヒドロピリミジニルベンズアゼピンジカルボキサミド化合物
EP3774806A1 (en) 2018-04-13 2021-02-17 GlaxoSmithKline Biologicals SA Tlr7 and / or tlr8 agonists
BR112020026890A2 (pt) 2018-07-03 2021-03-30 Jiangsu Hengrui Medicine Co., Ltd. Derivado de piridopirimidina, método de preparação do mesmo e uso médico do mesmo
US20210353737A1 (en) 2018-07-23 2021-11-18 Japan As Represented By Director General Of National Institute Of Infectious Diseases Composition containing influenza vaccine
KR20220018503A (ko) * 2019-05-23 2022-02-15 더 유니버시티 오브 몬타나 Tlr 수용체 리간드에 기반한 백신 애주번트
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KR102549083B1 (ko) 2021-02-01 2023-06-29 주식회사 에이티솔루션 레이다 전자 표적 발생 장치에서 발생되는 표적의 거리를 최소화하는 전파 지연 장치 및 방법

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Also Published As

Publication number Publication date
BR112012002349A2 (pt) 2015-10-13
EP2461690A4 (en) 2013-03-27
KR20120055623A (ko) 2012-05-31
EA023536B1 (ru) 2016-06-30
AU2010279299A1 (en) 2012-03-29
EP3199159B1 (en) 2019-04-10
CN102469790A (zh) 2012-05-23
AU2010279299B2 (en) 2015-10-01
WO2011017611A1 (en) 2011-02-10
TR201909600T4 (tr) 2019-07-22
JP2013501730A (ja) 2013-01-17
EP3199159A1 (en) 2017-08-02
SG178237A1 (en) 2012-03-29
JP5759992B2 (ja) 2015-08-05
US9044481B2 (en) 2015-06-02
ZA201200646B (en) 2013-06-26
ES2732999T3 (es) 2019-11-27
US20120135963A1 (en) 2012-05-31
CA2768195A1 (en) 2011-02-10
MX2012001524A (es) 2012-02-29
CN102469790B (zh) 2014-12-03
EP2461690A1 (en) 2012-06-13

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